4261-14-7Relevant articles and documents
Microwave assisted synthesis and biological activities of 9-boronobenzyladenine derivatives
Yu, Xue-Jun,Liu, Wei,Hu, Wei-Dong,Dong, Xue-Liang,Xu, Dan,Deng, You-Quan
, p. 347 - 349 (2007)
Microwave enhanced syntheses of 9-boronobenzyladenine derivatives by the reaction of adenine with the corresponding bromomethylphenylboric acid were reported. Microwave irradiation reduced the overnight reaction time of conventional thermal methods to 10
9-Hydroxymethylcyclopropylidenemethylenyladenine: The design, facile synthesis, isomer separation and Anti-HIV-1 activities
Cheng, Changmei,Shimo, Tetsuro,Somekawa, Kenichi,Baba, Masanori
, p. 2031 - 2040 (1998)
9-Hydroxymethylcyclopropylidenemethylenyladenine was designed based on the analysis of the structure-activity relationship and synthesized by coupling reaction of a vicinal dibromocyclopropane derivative with adenine. The cis/trans isomers and an enantiom
Lead optimization and biological evaluation of fragment-based cN-II inhibitors
Guillon, Rémi,Rahimova, Rahila,Preeti,Egron, David,Rouanet, Sonia,Dumontet, Charles,Aghajari, Nushin,Jordheim, Lars Petter,Chaloin, Laurent,Peyrottes, Suzanne
, p. 28 - 44 (2019/02/25)
The development of cytosolic 5′-nucleotidase II (cN-II) inhibitors is essential to validate cN-II as a potential target for the reversion of resistance to cytotoxic nucleoside analogues. We previously reported a fragment-based approach combined with molecular modelling, herein, the selected hit-fragments were used again in another computational approach based on the Ilib-diverse (a software enabling to build virtual molecule libraries through fragment based de novo design) program to generate a focused library of potential inhibitors. A molecular scaffold related to a previously identified compound was selected and led to a novel series of compounds. Ten out of nineteen derivatives showed 50–75% inhibition on the purified recombinant protein at 200 μM and among them three derivatives (12, 13 and 18) exhibited Ki in the sub-millimolar range (0.84, 2.4 and 0.58 mM, respectively). Despite their only modest potency, the cN-II inhibitors showed synergistic effects when used in combination with cytotoxic purine nucleoside analogues on cancer cells. Therefore, these derivatives represent a family of non-nucleos(t)idic cN-II inhibitors with potential usefulness to overcome cancer drug resistance especially in hematological malignancies in which cN-II activity has been described as an important parameter.
A new 9-alkyladenine-cyclic methylglyoxal diadduct activates wt- and F508del-cystic fibrosis transmembrane conductance regulator (CFTR) in vitro and in vivo
Boucherle, Benjamin,Bertrand, Johanna,Maurin, Bruno,Renard, Brice-Lo?c,Fortuné, Antoine,Tremblier, Brice,Becq, Frédéric,Norez, Caroline,Décout, Jean-Luc
, p. 455 - 465 (2014/07/21)
Cystic fibrosis transmembrane conductance regulator (CFTR) is the main chloride channel present in the apical membrane of epithelial cells and the F508 deletion (F508del-CFTR) in the CF gene is the most common cystic fibrosis-causing mutation. In the sear
